• Title/Summary/Keyword: Half-life(t1/2)

Search Result 250, Processing Time 0.022 seconds

Kinetics and Mechanism of Hydrolysis of Insecticidal Imidacloprid (살충성 Imidacloprid의 가수분해 반응 메카니즘)

  • Yu, Sung-Jae;Kang, Moon-Sung;Sung, Nack-Doo
    • Applied Biological Chemistry
    • /
    • v.40 no.1
    • /
    • pp.53-57
    • /
    • 1997
  • The rate of hydrolysis of insecticidal 1-(6-chloro-3-pyridylmethyl) -2-nitro-iminoimidazolidine (common name; imidacloprid) have been investigated in 15%(v/v) aqueous dioxane at $45^{\circ}C$. From the kinetics and non-kinetics data such as pH-effect, solvent effect(m=0.04, n=0.30 IT m<${\Delta}H^{\neq}=16.14kcal{\cdot}mol^{-1}\;&\;{\Delta}S^{\neq}=-0.03e.u.$), rate equation ($k_{obs.}=4.56{\times}10^{-3}[OH^-]$) and analysis of hydrolysis product, 1-(6-chloro-3-pyridylmethyl-2)-imidazolidinon, the hydrolysis mechanism of imidacloprid is proposed that the specific base catalyzed hydrolysis($K_{OH^-}$) through nucleophilic addition-elimination ($Ad_N-E$) mechanism proceed via intermediate, 1-(6-chloro-3- pyridylmethyl)-2-hydroxy-2-imidazolidinylisonitraminate (I) and ${\beta}$-3-(6-chloro-3-pyridylmethyl)aminoethyl-1-nitrourea(III). And the half-life(t1/2) of hydrolytic degradation at pH 8.0 and $45^{\circ}C$ was about 4.5 months.

  • PDF

Impact of Storage Temperature on Quality Characteristics and Oxidation Kinetic of Perilla Seed (저장온도가 들깨의 품질특성 및 산화속도에 미치는 영향)

  • Lee, Kyo-Yeon;Kim, Ah-Na;Rahman, M. Shafiur;Lee, Myoung Hee;Kim, Jung In;Kwak, Doyeon;Kim, Hyun-Jin;Choi, Sung-Gil
    • The Korean Journal of Food And Nutrition
    • /
    • v.32 no.6
    • /
    • pp.669-677
    • /
    • 2019
  • The impact of storage temperature on the changes in acid value(AV), peroxide value(POV), color value, total phenolic content(TPC), and antioxidant activity in perilla seed(PS) was investigated. The PS was stored at 25, 35, and 45℃ for four weeks. An increase in the storage temperature resulted in significantly increased AV, POV, redness, and yellowness of the PS. Conversely, TPC, antioxidant activity, and redness of the PS significantly decreased. The changes in the AV and POV followed a first-order kinetic model, and the kinetic parameters such as k, t1/2, Q10 and Ea were calculated. The k and t1/2 values decreased with increasing storage temperature and the Q10 values for the AV and POV were 1.56, 1.91, 4.61, and 3.43, respectively. The Ea for the changes in of the AV and POV in the PS were 70.40, 102.63 kJ/mol, respectively. The half-life values for the AV and POV of the PS at 25℃ were 169.52 and 373.18 days, respectively, while the values at 45℃ for those, were 28.47 and 27.93 days, respectively.

Evaluation of bioequivalence of two enrofloxacin formulations after intramuscular administration in goats

  • Aboubakr, Mohamed Hafez
    • Korean Journal of Veterinary Research
    • /
    • v.53 no.2
    • /
    • pp.77-82
    • /
    • 2013
  • The present study was planned to evaluate the bioequivalence of two commercial formulations of enrofloxacin, which have been marketed as 10% injectable solution after intramuscular administration at a single dose of 2.5 mg/kg body weight to 12 clinically healthy goats The study was carried out on the basis of crossover design. The two formulations were: Baytril as a reference product and Spectrama Vet as a test product. The plasma concentrations of enrofloxacin were measured by high performance liquid chromatography (HPLC) with UV detector. The pharmacokinetics of that data was performed using non-compartmental analysis. The maximum plasma concentration ($C_{max}$), time to reach peak concentration ($T_{max}$), area under concentration-time curve (AUC), elimination half-life ($t_{0.5el}$) were 1.14 and $1.05{\mu}g/mL$, 0.79 and 0.83 h, 5.70 and $5.79{\mu}g.h/mL$, 5.19 and 5.39 h for Baytril and Spectrama Vet, respectively. The 90% confidence interval for the mean ratio of $T_{max}$, $C_{max}$ and AUC were 94.72-116.2, 87.88-97.16 and 86.44-118.72%, respectively. These values falls within the European Medicines Agency bioequivalence acceptance range of 80-125% for both $T_{max}$ and AUC and between 75-133% for $C_{max}$. In conclusion, Spectrama-Vet is bioequivalent to Baytril and both products can be used as interchangeable drug in veterinary medicine practice.

Indocyanine green excretion test and changes of plasma enzyme activities in Korean native cattle and dairy cattle (한우 및 유우에서의 indocyanine green 배설시험 및 혈장효소 활성치의 변화)

  • Son, Min-soo;Kim, Cheol-ho;Choi, IL-kwan;Kim, Jin-gu;Hur, Ju-hyeong;Kang, Chung-boo
    • Korean Journal of Veterinary Research
    • /
    • v.32 no.4
    • /
    • pp.677-681
    • /
    • 1992
  • This experiment was carried out to establish a proper method of indocyanine green(ICG) excrection test for a applicable liver function test in three Korean native cattle average weighing about 450kg and dairy cattle parity of 3~5. The results obtained the half life($T^1/_2$), fractional clearance rate(KICG), retention rate and plasma enzyme activities before or after injection of ICG were as follows. 1. The maximum absorbance of ICG in plasma was at 805nm. 2. Average half life and fractional clearance rate following the injection of ICG 0.25mg/kg body weight were $5.53{\pm}1.27$ minute and $0.131{\pm}0.031$/minute in Korean native cattle, $4.55{\pm}0.68$ minute and $0.156{\pm}0.031$/minute in dairy cattle, respectively. The ICG removal rate was exponentially liner for the first 15 minutes after injection both of Korean native cattle and dairy cattle. 3. Average plasma retention rate when 10, 15, 30 minutes after injection was $35.7{\pm}13.9$, $23.2{\pm}7.1$, $10.8{\pm}3.5%$ in Korean native cattle, $26.8{\pm}3.3$, $14.2{\pm}1.2$, $5.5{\pm}2.2%$ in dairy cattle, respectively. 4. Plasma enzyme activities(AST, ALT, r-GTP) were no variation among the before, during and after injection of ICG. From these results, ICG excretion test to cattle is applicable to evaluation of liver funtion in both clinical and research, and adopted the 15 minutes plasma sample as the sample taken at the ideal time for comparative purposes.

  • PDF

HPLC Determination and Pharmacokinetic Profile of Warfarin in Korean Subjects (와파린의 HPLC 분석법 및 한국인에서의 약동학적 특징)

  • Bae, Jung-Woo;Kim, Hyun-Kyung;Yang, Sang-In;Kim, Ji-Hong;Kim, Kyung-Hye;Jang, Choon-Gon;Park, Young-Seo;Sohn, Uy-Dong
    • YAKHAK HOEJI
    • /
    • v.49 no.2
    • /
    • pp.134-139
    • /
    • 2005
  • Warfarin is a widely used oral anticoagulant agent used to treat thromboembolic disease. The purpose of this study was to develop the efficient assay method of warfarin sodium i n human plasma and to assess the pharmacokinetic profile of the warfarin in healthy Korean volunteers. The pharmacokinetics of warfarin administered orally was evaluated after a dose of 10 mg. Warfarin in plasma was assayed using a specific HPLC method with UV absorbance at 304 nm. AUC was 46.33${\pm}9.95{\mu}g/ml.hr$, $C_{max}$ $1.22{\pm}0.22{\mu}g/ml, $T_{max}$$2.50{\pm}1.41$ hr and half-life $43.49{\pm}4.33$ hr. $T_{max}$ was slightly shorter than that in Caucasian (3~9 hr), whereas the half-life was longer than that in Caucasian (10~45 hr, mean: 36 hr). These results suggest that warfarin may have a longer duration in Korean than in Caucasian.

Calpain Protease-dependent Post-translational Regulation of Cyclin D3 (Calpain protease에 의한 cyclin D3의 post-translation조절)

  • Hwang, Won Deok;Choi, Yung Hyun
    • Journal of Life Science
    • /
    • v.25 no.1
    • /
    • pp.1-7
    • /
    • 2015
  • Cyclin D is a member of the cyclin protein family, which plays a critical role as a core member of the mammalian cell cycle machinery. D-type cyclins (D1, D2, and D3) bind to and activate the cyclin-dependent kinases 4 and 6, which can then phosphorylate the retinoblastoma tumor suppressor gene products. This phosphorylation in turn leads to release or derepression of E2F transcription factors that promote progression from the G1 to S phase of the cell cycle. Among the D-type cyclins, cyclin D3 encoded by the CCND3 gene is one of the least well studied. In the present study, we have investigated the biochemistry of the proteolytic mechanism that leads to loss of cyclin D3 protein. Treatment of human prostate carcinoma PC-3-M cells with lovastatin and actinomycin D resulted in a loss of cyclin D3 protein that was completely reversible by the peptide aldehyde calpain inhibitor, LLnL. Additionally, using inhibitors for various proteolytic systems, we show that degradation of cyclin D3 protein involves the $Ca^{2+}$-activated neutral protease calpain. Moreover, the half-life of cyclin D3 protein half-life increased by at least 10-fold in PC-3M cells in response to the calpain inhibitor. We have also demonstrated that the transient expression of the calpain inhibitor calpastatin increased cyclin D3 protein in serum-starved NIH 3T3 cells. These data suggested that the function of cyclin D3 is regulated by $Ca^{2+}$-dependent protease calpain.

GET Imaging Evaluation of Patients with Esophageal Cancer (식도암 환자의 GET 영상 평가)

  • Moon, Jong Wun;Lee, Chung Wun;Seo, Young Deok;Yun, Sang Hyeok;Kim, Yong Keun;Won, Woo Jae
    • The Korean Journal of Nuclear Medicine Technology
    • /
    • v.17 no.2
    • /
    • pp.31-36
    • /
    • 2013
  • Purpose: Measure gastric emptying time (GET: Gastric Emptying Time) is a non-invasive and quantitative evaluation methods, mainly by endoscopic or radiological examination confirmed no mechanical obstruction in patients with symptoms of congestion is checked. Such tests are not common gastric emptying time measured esophageal cancer patients (who underwent esophagectomy) patients after surgery for gastric emptying time was measured test. And the period of time for more than one year after the gastric emptying time measurement was performed. By comparing the two kinds of tests in the chest cavity after surgery as the evaluation of gastrointestinal function tests evaluate the usefulness of GET, and will evaluate the characteristics of the image. Materials and Methods: 93 patients who underwent esophagectomy with gastric emptying time measurement of subject tests immediately after surgery and after 1 year or longer were twice. Preparation of the patient before the test is more than 12 hours of overnight fasting is important, in addition to the medicine or to stop smoking, and diabetes insulin injections should be early in the morning is ideal to test. Generally labeled with $^{99m}Tc-DTPA$ resin which is used to make steamed egg, seaweed and fermented milk with a high viscosity after eating, three hours in the standing position was measured. Evaluation of gastric emptying curves on the way intragastric radioactivity level by 50% the time (half-time [T1/2]) was calculated, based on the half-life was divided into three steps: over 180 minutes was defined as delayed gastric emptying, within 180minutes was defined as intermediate gastric emptying and when all the radioisotopes were dumped into the jejunum as soon as swallowed, was defined as rapid gastric emptying. Results: Gastric emptying time of a typical images stomach of antrum and fundus additional images appear stronger over time move on to the small intestine. but esophageal cancer who underwent esophagectomy side of the thoracic cavity showed a strong image. Immediately after surgery, the half-time (T1/2) of rapid gastric emptying appeared to 12.9%, intermediate gastric emptying appeared to 52.7%, delay gastric emptying appeared to 34.4%. After more than a year the results of the half-life after surgery, 67% of rapid gastric emptying to intermediate gastric emptying was changed, 69% of delay gastric emptying to intermediate gastric emptying changed. Intermediate gastric emptying worse in patients rapid gastric emptying and the delay gastric emptying is 24% in the case. Conclusion: Esophagectomy for esophageal cancer who underwent half-time measurement test (T1/2) rapid gastric emptying and delay gastric emptying are the result of the comparison over time, changes were observed intermediate gastric emptying. Mainly seeing of gastric emptying time measurement in the esophagus instead of thoracic cavity to check the evaluation of gastrointestinal function can be useful even means. And segmentation criteria and narrow time interval of checking if more accurate information and analysis of the clinical diagnosis and evaluation seems to be done.

  • PDF

Pharmacokinetics and Bioavailability of New Synthetic 5-HT2C Agonists, KKHQ80109 and KKHQ80114, in Sprague-Dawley Rats

  • Im, Hye-Yeon;Choo, Hyun-Ah;Pae, Ae-Nim;Kwon, Oh-Seung
    • Journal of Pharmaceutical Investigation
    • /
    • v.39 no.5
    • /
    • pp.327-331
    • /
    • 2009
  • 5-HT$_{2C}$ receptors have been considered as therapeutic targets for the treatment of various central nervous system disorders such as depression, anxiety, epilepsy, schizophrenia and sleep disorders. We chemically synthesized KKHQ80109 (K09) and KKHQ80114 (K14), selective 5-HT$_{2C}$ agonists, with the purpose of developing therapeutic agents for the treatment of obesity. The objective of this work is to investigate pharmacokinetic parameters and bioavailability of K09 and K14 in rats given orally or intravenously. Oral administration of 20 mg/kg K09 results in 4.11 hr of the terminal half-life and 89.16 ng/mL of C$_{max}$ at 5.00 hr (T$_{max}$). The terminal half-life of K14 was 3.83 hr with 215.81 ng/mL of C$_{max}$ at 3.33 hr (T$_{max}$) after oral dosing of 20 mg/kg K14, indicating that K14 is more rapidly absorbed than K09. Bioavailability showed 0.17-0.21 for K09 and 0.19-0.23 for K14. Urinary excretion of parent K09 and K14 was less than 1%, indicating that K09 and K14 undergo very extensive hepatic metabolism.

Correlation Analysis Between Stomach Qi Deficiency Pattern and Gastric Emptying Measured by Abdominal Ultrasonography in Patients with Functional Dyspepsia (기능성소화불량에서 위기허증(胃氣虛證)과 복부초음파로 측정한 위 배출능과의 상관성 분석)

  • Nam, Seong-uk;Park, Jae-woo;Kim, Jin-sung
    • The Journal of Internal Korean Medicine
    • /
    • v.39 no.3
    • /
    • pp.405-425
    • /
    • 2018
  • Objective: The purpose of this study was to analyze the correlation between Stomach Qi Deficiency and gastric emptying as measured by abdominal ultrasonography in postprandial distress syndrome (PDS), a subgroup of functional dyspepsia (FD). Methods: Ten patients who met the Rome III diagnostic criteria for PDS and ten healthy controls participated in this study Gastric emptying shown as the half-life of gastric volume ($T_{1/2}$) was measured by abdominal ultrasonography. The degree of Stomach Qi Deficiency was assessed using the scale for Stomach Qi Deficiency pattern (SSQD). In addition, functional dyspepsia-related quality of life (FD-QoL), Nepean dyspepsia index-Korean version (NDI-K), and visual analogue scale (VAS) of distention and fullness were conducted on all subjects. Results: The scores of SSQD, FD-QoL, NDI-K, and VAS of distention and fullness in the patient group were significantly higher than those in the control group (p<0.05). $T_{1/2}$ was also higher in the patient group than in the control group. The SSQD score significantly correlated positively with $T_{1/2}$ in the patient group (r=0.640, p=0.046). However, there was no significant correlation between $T_{1/2}$ and other questionnaire scores in the patient group. Conclusions: Our results suggest that the gastric emptying measured by abdominal ultrasonography could be a quantitative indicator to diagnose Stomach Qi Deficiency in FD patients, especially the PDS subtype.

Indocyanine green excretion test and changes of plasma enzyme activites in dogs (개에서의 indocyanine green 배설시험 및 혈장효소 활성치의 변화)

  • Kim, Cheol-ho;Choi, Il-kwan;Son, Min-soo;Kim, Jin-gu;Kang, Chung-boo
    • Korean Journal of Veterinary Research
    • /
    • v.32 no.4
    • /
    • pp.671-675
    • /
    • 1992
  • This experiment was carried out to establish a proper method of indocyanine green(ICG) excretion test for a applicable liver function test in dogs. The half life(T1/2), fractional clearance rate(KICG) and retention rate after injection of ICG with or without administred carbon tetrachloride($CCl_4$) were also invested. The results obtained were as follows ; 1. The maximum absorbance of ICG in plasma was at 810nm. 2. Half life and fractional clearance rate when administered 0.25 and 0.50mg of ICG per Kilogram body weight were $6.33{\pm}0.58$ minutes and $0.11{\pm}0.99$/minute in the former, $10.01{\pm}1.0$ minutes and $0.07{\pm}0.007$/minute in the latter, respectively. The ICG removal rate was exponentially linear for the first 15 minutes after injection both, of 0.25 and 0.50mg of ICG. 3. One day following the administration of $0.0042m{\ell}\;CCl_4$ kilogram body weight which injected 0.50mg of ICG, half life was more longer and fractional clearance rate was significantly reduced than that of ICG single injection. 4. Plasma retention rate when 15, 30, 45 minutes after injection dose of 0.25 and 0.50mg ICG per Kilogram body weight, $14.7{\pm}4.8$, $5.1{\pm}3.1$, $2.6{\pm}1.6%$ in the former, $26.9{\pm}1.8$, $11.1{\pm}2.4$, $4.8{\pm}1.3%$ in the latter, respectively. However, after administration of $CCl_4$, plasma retention rate of ICG at a dose of 0.50mg, it was $39.3{\pm}0.9$, $16{\pm}2.9$, $10.7{\pm}0.1%$, respectively. 5. Plasma enzyme(AST, ALT, r-GTP) activities administered with $CCl_4$ were increased, but there was no change which injected any dose of single ICG injection. From these results, ICG excretion test to dog is applicable to evaluation of liver function in both clinical and research.

  • PDF